|Targets||Polo-like Kinase (PLK)|
|Description||TAK-960 is an orally available PLK1 inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor TAK-960 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressed tumor cells. PLK1, named after the polo gene of Drosophila melanogaster, is a serine/threonine kinase crucial in the regulation of mitosis.|
|Synonyms||TAK 960; TAK960|
|Current Developer||Millennium Pharmaceuticals, Inc./Takeda Pharmaceutical Company Limited|
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BI 6727 (Volasertib) is a small highly potent Polo-like kinase inhibitor (Plk) with an IC50 of 0 .87 nM and EC50 of 11-37 nM on a panel of cancer cell lines, w...
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TAK-960 is an orally available PLK1 inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor TAK-960 selectively inhibits PLK1, inducing ...
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Rigosertib, a synthetic benzyl styryl sulfone, is a non-ATP-competitive inhibitor of PLK1 (IC50=9 nM).
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